Aceclofenac is a non-steroidal anti-inflammatory drug (NSAID) with marked anti-inflammatory and analgesic properties. It is reported to have a higher anti-inflammatory action or at least comparable effects than conventional NSAIDs in double-blind studies
Aceclofenac potently inhibits the cyclooxygenase enzyme (COX) that is involved in the synthesis of prostaglandins, which are inflammatory mediators that cause pain, swelling, inflammation, and fever. It is orally administered for the relief of pain and inflammation in osteoarthritis, rheumatoid arthritis, and ankylosing spondylitis. Aceclofenac belongs to BCS Class II as it possesses poor aqueous solubility. It displays high permeability to penetrate into synovial joints wherein patients with osteoarthritis and related conditions, the loss of articular cartilage in the area causes joint pain, tenderness, stiffness, crepitus, and local inflammation.
Aceclofenac belongs to the class of non-steroidal anti-inflammatory preparations for topical use. Used in the treatment of joint and muscular pains due to it muscle relaxing action.
Mechanism of Action of Aceclofenac
Through COX-2 inhibition, aceclofenac downregulates the production of various inflammatory mediators including prostaglandin E2 (PGE2), IL-1β, and TNF from the arachidonic acid (AA) pathway. Inhibition of IL-6 is thought to be mediated by diclofenac converted from aceclofenac. The suppressed action of inflammatory cytokines decreases the production of reactive oxygen species. Aceclofenac is shown to decreased production of nitrous oxide in human articular chondrocytes. In addition, aceclofenac interferes with neutrophil adhesion to endothelium by decreasing the expression of L-selectin (CD62L), which is a cell adhesion molecule expressed on lymphocytes. Aceclofenac is proposed to stimulate the synthesis of glycosaminoglycan in human osteoarthritic cartilage which may be mediated through its inhibitory action on IL-1 production and activity. The chondroprotective effects are generated by 4′-hydroxyaceclofenac which suppresses IL-1 mediated production of matrix metalloproteinase-1 and metalloproteinase-3 and interferes with the release of proteoglycan from chondrocytes
Indications of Aceclofenac
- Indicated for the relief of pain and inflammation in osteoarthritis, rheumatoid arthritis, and ankylosing spondylitis.
- Muscles stiffness in spinal
- Muscles stiffness in muscle diseases
- Muscles stiffness in the joint diseases
- Lumbago
- Low back pain
- PLID
- Frozen shoulder
- Ankylosing spondylitis
- Pain caused by nonarticular rheumatism
- Muscles stiffness in nerve diseases
- Rheumatoid arthritis
- Osteoarthritis
- Cervical spondylosis
- Periarthritis of scapulohumeral
- Ischiadynia
- a backache
- Teething
Contra-Indications of Aceclofenac
- Active peptic ulcer
- Acute rhinitis
- Allergic to thiocolchicoside
- Asthma
- Breastfeeding
- Pregnant
- Urticaria
- Concurrent peptic ulcer, or history of ulcer disease
- Allergy to indometacin, aspirin, or other NSAIDs
- Patients with nasal polyps reacting with an angioedema to other NSAIDs
- Children under 2 years of age (with the exception of neonates with patent ductus arteriosus)
- Some painkillers, including opioid pain killers;
- Hypnotic drugs;
- Psychotropic drugs;
- Used monoamine oxidase inhibitors (MAOIs) such as phenelzine or tranylcypromine
- Epilepsy;
- Addiction or are recovering from addiction to another medication.
- History of peptic ulcer disease,
- Gastrointestinal bleeding,
- Severe pre-existing renal and liver damage
- Caution: pre-existing bone marrow damage (frequent blood cell counts are indicated)
- Caution: bleeding tendencies of unknown origin
- Caution: Parkinson’s disease, epilepsy, psychotic disorders (indometacin may worsen these conditions)
- Concurrent with potassium sparing diuretics
- Patients who have a patent ductus arteriosus dependent heart defect (such as transposition of the great vessels)
- Significant hypertension (high blood pressure)
- Concomitant administration of lithium salts (such as lithium carbonate)
Dosage of Aceclofenac
Strengths : 100 mg , 200 mg
Ankylosing spondylitis
- 100 mg bid, in the morning and in the evening.
Rheumatoid arthritis
- 100 mg bid, in the morning and in the evening.
Osteoarthritis
- 100 mg bid, in the morning and in the evening.
Side Effects of Aceclofenac
The most common
- GI disorders (e.g. dyspepsia, abdominal pain, nausea, vomiting, diarrhoea, flatulence, constipation,, ulcerative stomatitis, ), indigestion,
- Disturbances of the gut such as diarrhoea, constipation, nausea, vomiting or abdominal pain.
- Drowsiness and lightheadedness
- Nausea and vomiting
- joint pain
- Nausea and vomiting
- Severe stomach ache
- Severe diarrhea
- Vaginal thrush
- Skin rash
- Headache
- Chest pain
- Diarrhea or loose stools
- Difficulty with breathing
- Dizziness
- Heartburn
- Muscle pain
More common
- Abdominal or stomach pain,
- Chills or fever
- Headache,
- Joint or back pain
- Muscle aching or cramping
- Muscle pains or stiffness
- Chest pressure or squeezing pain in the chest
- Excessive sweating
- feeling of heaviness, pain, warmth and/or swelling in a leg or in the pelvis
- sudden tingling or coldness in an arm or leg
- Constipation
- Diarrhoea
- Loss of muscle coordination
- Sleepiness or unusual drowsiness
- Clumsiness or unsteadiness
- Drowsiness
Rare
- Anxiety
- change in vision
- seizures
- abnormal or fast heart rate
- weight loss
- chest pain or tightness
- confusion
- a cough
- Agitation
- arm, back, or jaw pain
- blurred vision
- chest pain or discomfort
- convulsions
- extra heartbeats, fainting
- blurred vision
- chest pain or discomfort
- convulsions
- extra heartbeats
- hallucinations
- a headache
- irritability
- lightheadedness
- mood or mental changes
- muscle pain or cramps
- muscle spasm or jerking of all extremities
- muscle pains or stiffness
- chest pressure or squeezing pain in the chest
- discomfort in arms, shoulders, neck or upper back
- pain or discomfort in the chest, upper stomach, or throat
- pale or blue lips, fingernails, or skin
- puffiness or swelling of the eyelids or around the eyes, face, lips, or tongue
- unusual drowsiness, dullness, or feeling of sluggishness
Drug Interactions of Aceclofenac
Aceclofenac may interact with following drugs, supplyments & may change the efficacy of drugs
- antacids (e.g., aluminum hydroxide, calcium carbonate, magnesium hydroxide)
- bisphosphonates (e.g., alendronate, etidronate, risedronate, zoledronic acid)
- antipsychotics (e.g., chlorpromazine, clozapine, haloperidol, olanzapine, quetiapine, risperidone)
- angiotensin converting enzyme inhibitors (ACEIs; e.g., captopril, enalapril, ramipril)
- angiotensin receptor blockers (ARBs; e.g., candasartan, irbesartan, losartan)
- beta-adrenergic blockers (e.g., metoprolol, atenolol)
- baclofen
- barbiturates (e.g., butalbital, phenobarbital)
- benzodiazepines (e.g., alprazolam, diazepam, lorazepam)
- calcium channel blockers (e.g., amlodipine, diltiazem, nifedipine, verapamil)
- celecoxib
- cilostazol
- “azole” antifungals (e.g., itraconazole, ketoconazole, voriconazole)
- clopidogrel
- corticosteroids (e.g., dexamethasone, hydrocortisone, prednisone)
- cyclosporine
- diuretics (water pills; e.g., furosemide, hydrochlorothiazide, triamterene)
- 5-ASA medications (e.g, sulfasalazine)
- glucosamine
- haloperidol
- heparin
- methotrexate
- multivitamins
- other non-steroidal anti-inflammatory medications (NSAIDs;e.g., diclofenac, ibuprofen, ketorolac, naproxen)
- Omega-3 fatty acids
- phenytoin
- phenobarbital
- pentoxifylline
- quinolone antibiotics (e.g., ciprofloxacin, ofloxacin)
- selective serotonin reuptake inhibitors (SSRIs; e.g., citalopram, duloxetine, fluoxetine, paroxetine, sertraline)
- serotonin/norepinephrine reuptake inhibitors (SNRIs; e.g., duloxetine, venlafaxine)
- tricyclic antidepressants (e.g., amitriptyline, clomipramine, desipramine, trimipramine)
- warferin
Other NSAIDs: Concomitant therapy with aspirin or other NSAIDs may increase the frequency of adverse reactions, including the risk of GI bleeding.
Pregnancy& Lactation of Aceclofenac
FDA Pregnancy Category C
Pregnancy
There is no information on the secretion of aceclofenac in breast milk. The use of aceclofenac should therefore be avoided during lactation unless the potential benefits to the mother outweigh the possible risks to the children. During the third trimester of pregnancy, all prostaglandin synthesis inhibitors may expose the foetus to
- cardiopulmonary toxicity (with premature closure of the ductus arteriosus and pulmonary hypertension);
- renal dysfunction, which may progress to renal failure with oligo-hydramnios;
the mother and the neonate, at the end of pregnancy, to
- possible prolongation of bleeding time, an anti-aggregating effect which may occur even at very low doses.
- inhibition of uterine contractions resulting in delayed or prolonged labor.
Consequently, aceclofenac is contraindicated during the third trimester of pregnancy
Lactation
There is no information on the secretion of aceclofenac to breast milk; there was, however, no notable transfer of radiolabelled aceclofenac to the milk of lactating rats. The use of aceclofenac should, therefore, be avoided in pregnancy and lactation unless the potential benefits to the other outweigh the possible risks to the fetus.
